antimalarial, anti-parasitic and anthelmintics agents
Lumefantrine
brand name coartem
( mixed with arthemeter)
Arthemether
brand name coartem
(mixed with lumefantrine
Atovaquone-progaunil
Artesunate(brand name Artesun)
chlroquine phosphate
Property
side effects
headache, anorexia, dizziness, and asthenia.
caution
Severe renal and hepatic impairment. Children. Pregnancy and lactation. .
adme
Absorption: dependant of coadministration of fat
Excretion: half life of 3 to 6 days
dose
( with arthemether) Each tab contains artemether 20 mg and lumefantrine 120 mg: ≥35 kg: Initial: 4 tab, followed by 4 tab given at 8, 24, 36, 48, and 60 hours thereafter to a total of 24 tab over 3 days.
indications
-the treatment of acute uncomplicated malaria caused by Plasmodium falciparum, including malaria acquired in chloroquine-resistant areas.
MOA
-inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
SIDE EFFECTS
headache, anorexia, dizziness, and asthenia.
CAUTION
- do not take during pregnancy or lactation
ADME
Metabolism: Rapidly hydrolysed to the active metabolite dihydroartemisinin.
Excretion: Elimination half-life: about 4-11 hr after IM or oral admin.
DOSE
- 80 mg/day. Take doses at diagnosis and
repeat after 8, 24, 36, 48 and 60 hr
Indications
treatment of chroquine-resistant falciparum malaria and complicated falciparum malaria
MOA
Involves an interaction with ferriprotoporphyrin IX (“heme”),or ferrous ions, in the acidic parasite food vacuole,
which results in the generation
of cytotoxic radical species.
MOA: cleavage of endoperoxide bridge in the pharmacophore of DHA generates reactive oxygen species (ROS), which increases oxidative stress and causes malarial protein damage via alkylation.
Indication: first line treatment for children or adults with severe malaria.
ADME: absorbtion is good and mec is within 8 to 15 minutes.Distribution is in body fluids as it binds 93 percent to plasma protein. metabolises by plasma esterases to form its active ingridient DHA. elimination is urine and feces.
Adverse effect: Cardiotoxicity (high doses),
Neurotoxicity , drug induce fever, skin rash.
Side effect: anemia, low rbc and platelet count,
swelling of liver
precaution: pregnant and lactation should not take
Dose: oral is 5mg/kg followed by 2.5mg/kg for both adult an children above 6 months.
: parental is 2mg/kg loading dose followed by 1mg/kg
every 4 hours for maximum of 1 week.
combination therapy: take with Pyrimethamine and mefloquine.
Pharmacology
Odorless
Bitter taste
Slightly soluble in water and insoluble in alcohol
Rapidly and almost completely absorbed from the GI tract
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Excretion is slow but increased by acidification of urine
Only small amount of it found in stool
55% of drug in the plasma is bounded to nondiffusable plasma constituents
Indication
Suppressive treatment and for acute attack of malaria due to P.vivax, P.malariae, P.ovale and susceptible P.falciparum.
Extraintestinal amebiasis
Not effective against exoerythrocytic forms of parasite
Contraindication
Presence of retinal or visual field change
Serious adverse reaction in nursing infants
Pregnant women who are nursing infants, infants who are less than 5kg and people with severe kidney disease
Drug interaction
Is actually a combination of two drugs in a single tablet
Increased risk for bleeding if take with Coumadin, a blood-thinner
Side effects
Stomach pain
Nausea
Vomitting
Side effects can be lessened if taken with food
Other considerations
Good for last minute travelers because the drug is started 1-2 days before travelling to malaria area
Good choice for sorter trips because you only have to take the medicine for 7 days after travelling rather than 4weeks
More expensive
Used for
Prophylaxis of Plasmodium falciparum malaria
Treatment of acute, uncomplicated Plasmodium falciparum malaria